Indiplon

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Hypnotic sedative drug

title: "Indiplon" type: doc version: 1 created: 2026-02-28 author: "Wikipedia contributors" status: active scope: public tags: ["hypnotics", "pyrazolopyrimidines", "sedatives", "diarylketones", "thiophenes", "acetanilides", "gabaa-receptor-positive-allosteric-modulators"] description: "Hypnotic sedative drug" topic_path: "general/hypnotics" source: "https://en.wikipedia.org/wiki/Indiplon" license: "CC BY-SA 4.0" wikipedia_page_id: 0 wikipedia_revision_id: 0

::summary Hypnotic sedative drug ::

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Indiplon (INN and USAN) is a unmarketed nonbenzodiazepine, hypnotic sedative that was developed in two formulations—an immediate-release formulation for sleep onset, and a modified-release (also called controlled-release or extended-release) version for sleep maintenance.

Pharmacology

Pharmacodynamics

Indiplon works by enhancing the action of the inhibitory neurotransmitter GABA, like most other nonbenzodiazepine sedatives. It primarily binds to benzodiazepine sites on α1 subunit-containing GABAA receptors in the brain.

Pharmacokinetics

Indiplon has a short elimination half-life of 1.5 to 1.8 hours in young and elderly subjects, respectively.

Chemistry

Indiplon is a pyrazolopyrimidine related to the nonbenzodiazepine hypnotic zaleplon.

History

Indiplon was discovered at Lederle Laboratories (which was later acquired by Wyeth) in the 1980s and was called CL 285,489. In 1998 Lederle licensed it, along with other early stage drug candidates, to DOV Pharmaceutical, a startup formed by former Lederle employees, and Dov exclusively sublicensed its rights in the drug to Neurocrine Biosciences in that same year. In 2002, Neurocrine entered into an agreement with Pfizer to develop the drug.

Indiplon was originally scheduled for release in 2007, when Sanofi-Aventis' popular hypnotic zolpidem lost its patent rights in the United States and thus became available as a much less expensive generic. In 2002, Neurocrine Biosciences had entered into an agreement with Pfizer to co-market indiplon in the US, in a deal worth a potential $400mn. However, following the issuing of a non-approvable letter for the modified-release 15 mg formulation and an approvable letter with stipulations for the 5 mg and 10 mg immediate-release version by the FDA in May 2006, Pfizer ended its relationship with Neurocrine. Neurocrine's stock price dropped 60% on the news.

Following a resubmission, the FDA in December 2007 deemed Neurocrine's new drug application (NDA) 'approvable' in the 5 and 10 mg formulations,{{cite press release | title = Neurocrine Receives Approvable Letter for Indiplon Capsules with Additional Safety and Efficacy Data Required by FDA | publisher = Neurocrine Biosciences, Inc. | date = 2007-12-13 | url = https://www.drugs.com/nda/indiplon_071213.html | access-date = 2007-12-13

Following the 2007 FDA letter, Neurocrine decided to discontinue all clinical and marketing development of Indiplon in the United States.

References

References

  1. (April 2006). "Indiplon is a high-affinity positive allosteric modulator with selectivity for alpha1 subunit-containing GABAA receptors". The Journal of Pharmacology and Experimental Therapeutics.
  2. (September 2009). "Indiplon in the management of insomnia". Drug Design, Development and Therapy.
  3. (November 2004). "Characterization of the interaction of indiplon, a novel pyrazolopyrimidine sedative-hypnotic, with the GABAA receptor". The Journal of Pharmacology and Experimental Therapeutics.
  4. (2010). "GABA and Sleep: Molecular, Functional and Clinical Aspects.". Springer Science & Business Media.
  5. (18 June 2010). "San Diego's Neurocrine Biosciences Scores Second Big Deal in Two Days". [[The Motley Fool]].
  6. (16 May 2006). "Neurocrine's FDA Nightmare". TheStreet.com.
  7. (22 June 2006). "Pfizer Drops Neurocrine Deal". TheStreet.com.
  8. (15 May 2006). "Neurocrine stock price plunges 60 percent:FDA's mixed review of sleeping pill Indiplon could threaten Pfizer-Neurocrine partnership". CNN Money.
  9. (2012-02-16). "Additional Pipeline Projects". Neurocrine.

::callout[type=info title="Wikipedia Source"] This article was imported from Wikipedia and is available under the Creative Commons Attribution-ShareAlike 4.0 License. Content has been adapted to SurfDoc format. Original contributors can be found on the article history page. ::

hypnoticspyrazolopyrimidinessedativesdiarylketonesthiophenesacetanilidesgabaa-receptor-positive-allosteric-modulators